Hydroxyfasudil
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MedKoo CAT#: 526102

CAS#: 105628-72-6 (free base)

Description: Hydroxy-Fasudil is a metabolite of Fasudil, acting as a potent Rho-kinase inhibitor and vasodilator.

Chemical Structure

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Hydroxyfasudil
CAS# 105628-72-6 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 526102
Name: Hydroxyfasudil
CAS#: 105628-72-6 (free base)
Chemical Formula: C14H17N3O3S
Exact Mass: 307.10
Molecular Weight: 307.368
Elemental Analysis: C, 54.71; H, 5.58; N, 13.67; O, 15.62; S, 10.43

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
25mg USD 650 2 Weeks
50mg USD 950 2 Weeks
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Related CAS #: 155558-32-0 (HCl)   105628-72-6 (free base)  

Synonym: Hydroxyfasudil

IUPAC/Chemical Name: 5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one

InChi Key: ZAVGJDAFCZAWSZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H17N3O3S/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17/h1,3-5,7,15H,2,6,8-10H2,(H,16,18)

SMILES Code: O=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 307.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Ray P, Wright J, Adam J, Boucharens S, Black D, Brown AR, Epemolu O, Fletcher D, Huggett M, Jones P, Laats S, Lyons A, de Man J, Morphy R, Sherborne B, Sherry L, Straten Nv, Westwood P, York M. Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1084-8. doi: 10.1016/j.bmcl.2010.12.104. Epub 2010 Dec 28. PubMed PMID: 21251828.

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3: Huang L, Li Q, Li H, He Z, Cheng Z, Chen J, Guo L. Inhibition of intracellular Ca2+ release by a Rho-kinase inhibitor for the treatment of ischemic damage in primary cultured rat hippocampal neurons. Eur J Pharmacol. 2009 Jan 14;602(2-3):238-44. doi: 10.1016/j.ejphar.2008.11.053. Epub 2008 Dec 3. PubMed PMID: 19070614.

4: Hinderling PH, Karara AH, Tao B, Pawula M, Wilding I, Lu M. Systemic availability of the active metabolite hydroxy-fasudil after administration of fasudil to different sites of the human gastrointestinal tract. J Clin Pharmacol. 2007 Jan;47(1):19-25. PubMed PMID: 17192498.

5: Scherer EQ, Arnold W, Wangemann P. Pharmacological reversal of endothelin-1 mediated constriction of the spiral modiolar artery: a potential new treatment for sudden sensorineural hearing loss. BMC Ear Nose Throat Disord. 2005 Nov 29;5:10. PubMed PMID: 16316469; PubMed Central PMCID: PMC1315339.

6: Sato S, Ikegaki I, Asano T, Shimokawa H. Antiischemic properties of fasudil in experimental models of vasospastic angina. Jpn J Pharmacol. 2001 Sep;87(1):34-40. PubMed PMID: 11676196.

7: Satoh S, Utsunomiya T, Tsurui K, Kobayashi T, Ikegaki I, Sasaki Y, Asano T. Pharmacological profile of hydroxy fasudil as a selective rho kinase inhibitor on ischemic brain damage. Life Sci. 2001 Aug 10;69(12):1441-53. PubMed PMID: 11531167.

8: Satoh S, Kobayashi T, Hitomi A, Ikegaki I, Suzuki Y, Shibuya M, Yoshida J, Asano T. Inhibition of neutrophil migration by a protein kinase inhibitor for the treatment of ischemic brain infarction. Jpn J Pharmacol. 1999 May;80(1):41-8. PubMed PMID: 10446755.